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Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation | |
Qi, Wei; Chan, HoMan; Teng, Lin; Li, Ling; Chuai, Shannon; Zhang, Ruipeng; Zeng, Jue; Li, Min; Fan, Hong; Lin, Ying | |
2012 | |
发表期刊 | PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA |
ISSN | 0027-8424 |
卷号 | 109期号:52页码:21360-21365 |
发表状态 | 已发表 |
DOI | 10.1073/pnas.1210371110 |
摘要 | Ezh2 (Enhancer of zeste homolog 2) protein is the enzymatic component of the Polycomb repressive complex 2 (PRC2), which represses gene expression by methylating lysine 27 of histone H3 (H3K27) and regulates cell proliferation and differentiation during embryonic development. Recently, hot-spot mutations of Ezh2 were identified in diffused large B-cell lymphomas and follicular lymphomas. To investigate if tumor growth is dependent on the enzymatic activity of Ezh2, we developed a potent and selective small molecule inhibitor, EI1, which inhibits the enzymatic activity of Ezh2 through direct binding to the enzyme and competing with the methyl group donor S-Adenosyl methionine. EI1-treated cells exhibit genome-wide loss of H3K27 methylation and activation of PRC2 target genes. Furthermore, inhibition of Ezh2 by EI1 in diffused large B-cell lymphomas cells carrying the Y641 mutations results in decreased proliferation, cell cycle arrest, and apoptosis. These results provide strong validation of Ezh2 as a potential therapeutic target for the treatment of cancer. |
URL | 查看原文 |
收录类别 | SCI |
WOS研究方向 | Science & Technology - Other Topics |
WOS类目 | Multidisciplinary Sciences |
WOS记录号 | WOS:000313627700051 |
WOS关键词 | EMBRYONIC STEM-CELLS ; HISTONE H3 ; LYSINE 27 ; DEVELOPMENTAL REGULATORS ; SOMATIC MUTATIONS ; B-CELLS ; POLYCOMB ; GENE ; LYMPHOMA ; CANCER |
原始文献类型 | Article |
引用统计 | |
文献类型 | 期刊论文 |
条目标识符 | https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/120271 |
专题 | 个人在本单位外知识产出 |
共同第一作者 | Chan, HoMan |
通讯作者 | Li, En |
作者单位 | 1.China Novartis Inst BioMed Res, Shanghai 201203, Peoples R China 2.Novartis Inst BioMed Res, Ctr Prote Chem, Cambridge, MA 02139 USA |
推荐引用方式 GB/T 7714 | Qi, Wei,Chan, HoMan,Teng, Lin,et al. Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA,2012,109(52):21360-21365. |
APA | Qi, Wei.,Chan, HoMan.,Teng, Lin.,Li, Ling.,Chuai, Shannon.,...&Li, En.(2012).Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation.PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA,109(52),21360-21365. |
MLA | Qi, Wei,et al."Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation".PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA 109.52(2012):21360-21365. |
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